Preparation and applications of Doxorubicin-loading active targeting albumin nanometer carrier

A technology of albumin nanoparticles and albumin nanoparticles, which is applied in the field of anti-tumor targeted drug research to achieve the effects of ensuring activity, reducing immunogenicity, and improving targeting

Inactive Publication Date: 2016-02-03
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

The method used in the present invention to prepare albumin nanoparticles is a desolvation method, and the adsorption and connection of ant...

Method used

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  • Preparation and applications of Doxorubicin-loading active targeting albumin nanometer carrier
  • Preparation and applications of Doxorubicin-loading active targeting albumin nanometer carrier
  • Preparation and applications of Doxorubicin-loading active targeting albumin nanometer carrier

Examples

Experimental program
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Embodiment 1

[0032] (1) Prepare doxorubicin-loaded nanoparticles: dissolve 40 mg of albumin in 2 ml of water and pass through a 0.22 μm filter; add 800 μl of 0.5% doxorubicin hydrochloride solution, then add 0.05 mol / LpH9 sodium carbonate-sodium bicarbonate Buffer 1.2ml, stirred at room temperature for 2h. Then 16ml of absolute ethanol was added dropwise at a speed of 0.5ml / min with an infusion set, and 23μl of 25% glutaraldehyde solution was added to solidify for 16h. After solidification, the reaction solution was vacuum rotary evaporated at 45°C to remove ethanol, then ultrasonically dispersed with distilled water, centrifuged at 1,2000 rpm for 15 min, and the supernatant was discarded after centrifugation. Wash the centrifuged precipitate three times in the same way, and ultrasonically disperse with the same volume of distilled water each time. The obtained doxorubicin-loaded albumin nanoparticles (DOX-NPs) had an average particle size of 160.1 nm and a polydispersity coefficient of a...

Embodiment 2

[0035] (1) Add 300μl 250mM borax / 250mM sodium chloride and 300μl 100mM dithiothreitol (pH8.0) to 2.4ml cetuximab (5mg / ml), incubate at 37°C for 45min, desalt by ultrafiltration and centrifugation, and purify the reduced Antibody. Adjust the antibody concentration (2mg / ml), take 4ml, add MC-Val-Cit-PAB-DOX / DMF (5mg / ml) 0.6ml, let it stand on ice for 1h, add 490μl cysteine ​​(10mg / ml, containing Diethylenetriaminepentaacetic acid / PBS), and then rest for 45min. Desalting by ultrafiltration and centrifugation. Obtain the drug-antibody conjugate cetuximab-dipeptide doxorubicin (Cetuximab-vcDOX), measure the absorbance A280 and A495 of the drug-antibody conjugate at 280nm and 495nm by UV spectrophotometry, and pass the doxorubicin The standard curve at 280nm and 495nm of cetuximab and cetuximab calculates that the molar ratio of doxorubicin / cetuximab is 5.5, that is, 5.5 doxorubicin is connected to each cetuximab;

[0036] (2) Take 0.5 ml of 1% albumin solution, and slowly add 1....

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Abstract

The present invention discloses albumin nanoparticles, a preparation method and applications, wherein the albumin nanoparticles and an antibody or antibody drug conjugate (such as doxorubicin) are subjected to adsorption connection. According to the present invention, the experiment results show that: compared with the single drug, the nanoparticles modified with the antibody or antibody drug conjugate have advantages of enhancement of targeting property, and reduction of toxic-side effects of drugs on the body; and the formed albumin nanoparticles use the enhanced permeability and retention effect (EPR) of the tumor tissue to enhance the intratumoral accumulation so as to provide a certain slow release effect and a certain drug efflux inhibition effect, enhance the biological utilization rate of the drug, and reduce the drug consumption, such that the efficient and low-toxicity nanometer treatment way is provided for the tumor targeting therapy.

Description

technical field [0001] The invention belongs to the field of anti-tumor targeted drug research, and in particular relates to a preparation method and application of active targeting albumin nanoparticles loaded with doxorubicin. Background technique [0002] A major goal of cancer treatment is to develop drugs that are highly effective at killing tumor cells, but with as little toxicity as possible to normal tissues. One of the ways to improve selectivity and efficacy is to improve the targeting of drugs to tumors. Antigen-antibody system-mediated targeted therapy mainly uses the specific recognition mechanism between antigen and antibody to actively target drugs to specific cells to kill tumor cells. Many antibodies can recognize the specific antigens of most tumors such as liver cancer, ovarian cancer, colon cancer, etc. The main reason is the high expression of specific antigens on the surface of tumor cells. As a targeting ligand, monoclonal antibodies can effectively ...

Claims

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Application Information

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IPC IPC(8): A61K47/42A61K47/48A61K31/704A61P35/00
Inventor 涂家生张悦孙春萌吕杨格格
Owner CHINA PHARM UNIV
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